AIM: To investigate the altering expression profiles of efflux transporters such as breast cancer-resistance protein (BCRP), lung resistance protein (LRP), and multidrug resistance protein 1 (MDR1) at the inner blood-retinal barrier (BRB) during the development of early diabetic retinopathy (DR) and/or aging in mice. METHODS: Relative mRNA and protein expression profiles of these three efflux transporters in the retina during the development of early DR and/or aging in mice were examined. The differing expression profiles of Zonula occludens 1 (ZO-1) and vascular endothelial growth factor-A (VEGFA) in the retina as well as the perfusion characterization of fluorescein isothiocyanate (FITC)-dextran and Evans blue were examined to evaluate the integrity of the inner BRB. RESULTS: There were significant alterations in these three efflux transporters’ expression profiles in the mRNA and protein levels of the retina during the development of diabetes mellitus and/or aging. The development of early DR was confirmed by the expression profiles of ZO-1 and VEGFA in the retina as well as the compromised integrity of the inner BRB. CONCLUSION: The expression profiles of some efflux transporters such as BCRP, LRP, and MDR1 in mice retina during diabetic and/or aging conditions are tested, and the attenuated expression of BCRP, LRP, and MDR1 along with the breakdown of the inner BRB is found, which may be linked to the pathogenesis of early DR.